甲氨蝶呤柔性纳米脂质体凝胶的构建及体外经皮渗透性研究

目的 制备甲氨蝶呤(methotrexate,MTX)柔性纳米脂质体凝胶,并研究其体外经皮渗透行为.方法 采用逆向蒸发法制备MTX柔性纳米脂质体,以卡波姆940为基质制成脂质体凝胶,并考察其初步稳定性；Franz扩散池研究MTX柔性纳米脂质体凝胶与普通凝胶的经皮渗透规律.结果 脂质体凝胶4℃下稳定性良好；体外透皮试验表明,MTX柔性纳米脂质体凝胶的累积透过量明显＜MTX普通凝胶(P＜0.05),皮肤滞留量＞MTX普通凝胶(P＜0.05).结论 MTX柔性纳米脂质体凝胶可显著提高药物的皮肤滞留量,而不增加药物进入血液循环的量,能有效降低药物潜在的全身毒性,有望成为MTX局部治疗的新剂型.

Preparation of methotrexate flexible nano-liposome gel and its cutaneous permeation kinetics in vitro

Objective To prepare methotrexate(MTX) formable nano-liposome(MTX-FNL) gel and to study its cutaneous permeation kinetics in vitro.Methods The MTX-FNL was prepared by reverse evaporation method,and carbopol 940 was added as the base for the preparation of the liposemal gel.The Franz-diffusion cell was used to compare the permeation rate of MTX-FNL gel with MTX gel in vitro.Results The MTX-FNL gel was stable under 4 ℃.The cumulative penetration of MTX-FNL gel was higher than that of MTX gel(P<0.05),and cumulated amount in the skin was much higher than that of MTX gel(P<0.05).Conclusion MTX-FNL gel can increase the cumulated amount in the skin but can not increase the MTX content in the blood circulation,which effectively reduces the potential systemic toxicity and can be used as a carrier of MTX in the skin application.